CS-2265
中文名称 | CS-2265 |
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中文同义词 | GSK484盐酸盐;((3S,4R)-3-氨基-4-羟基哌啶-1-基)(2-(1-(环丙基甲基)-1H-吲哚-2-基)-7-甲氧基-1-甲基-1H-苯并[D]咪唑-5-基)甲酮盐酸盐;GSK484,可逆的PAD4抑制剂;GSK485 HYDROCHLORIDE;GSK484,PAD4抑制剂 |
英文名称 | GSK484 |
英文同义词 | GSK484;GSK484 (hydrochloride);CS-2265;PAD4 inhibitor GS484;GSK484 HCl;((3S,4R)-3-amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride;AOB6992;GTPL8577 |
CAS号 | 1652591-81-5 |
分子式 | C27H32ClN5O3 |
分子量 | 510.04 |
EINECS号 | |
相关类别 | 抑制剂;生化试剂 |
Mol文件 | 1652591-81-5.mol |
结构式 |
CS-2265 性质
储存条件 | 2-8°C |
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溶解度 | DMSO:25.0(最大浓度 mg/mL);49.01(最大浓度 mM) 乙醇:25.0(最大浓度 mg/mL);49.01(最大浓度 mM) PBS 缓冲液 (pH 7.2):5.0(最大浓度 mg/mL);9.8(最大浓度 mM) DMF:30.0(最大浓度 mg/mL);58.82(最大浓度 mM) |
形态 | 粉末 |
颜色 | 白色至米色 |
InChIKey | MULKOGJHUZTANI-JEGYXLSDNA-N |
SMILES | C(C1CC1)N1C2=CC=CC=C2C=C1C1=NC2=CC(C(N3CC[C@@H](O)[C@@H](N)C3)=O)=CC(OC)=C2N1C.Cl |&1:22,24,r| |
Target | Value |
PAD4
(in the absence of Calcium) | 50 nM |
GSK484 demonstrates high affinity binding to the low-calcium form of PAD4 with IC 50 s of 50 nM and 250 nM in the absence of Calcium (0 mM) and Calcium (2 mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2 mM Calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH 3 release assay.
To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4 mg/kg daily for one week. This dose suppress the elevated number of neutrophils undergoing NETosis in peripheral blood in mice with cancer. In parallel, the total protein level in urine from MMTV-PyMT mice is significantly reduced compared with untreated tumor-bearing mice, further supporting an improved functional status of the kidneys after GSK484 treatment. Administration of GSK484 at a dose of 4 mg/kg daily during one week reverts signs of kidney dysfunction in tumor-bearing mice to the same extent as DNase I treatment, without any detectable signs of toxicity.
安全信息
海关编码 | 2933399990 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/11/08 | S7803 | CS-2265 GSK484 HCl | 1652591-81-5 | 5mg | 2574.56元 |
2024/11/08 | HY-100514 | CS-2265 GSK484 hydrochloride | 1652591-81-5 | 5mg | 2100元 |